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Rostafuroxin

CAS No. : 156722-18-8

MCE 站：Rostafuroxin

产品活性：Rostafuroxin (PST 2238) 是一种洋地黄毒苷衍生物，一种口服有效的 Na⁺,K⁺-ATPase (ATP1A1) 抑制剂。Rostafuroxin 与 ATP1A1 胞外域特异性结合，并阻断呼吸道合胞病毒 (RSV) 触发的 EGFR Tyr845 磷酸化。Rostafuroxin 具有抗高血压和抗 RSV 活性。

研究领域：Membrane Transporter/Ion Channel  |  Anti-infection

作用靶点：Na+/K+ ATPase  |  RSV

In Vitro: Rostafuroxin (PST 2238) competitively inhibits Ouabain (HY-B0542) binding and signaling. Rostafuroxin antagonizes the molecularand functional effects of Ouabain by reversing the ouabain-induced, Src-dependent Na⁺,K⁺-ATPase phosphorylation and activation.
Rostafuroxin (0.125-128 μM; for 24 h post treatment) has less than 20% reduction in cell viability in A549 cells and HSAEC. Rostafuroxin inhibits the expression of RSV-GFP in HSAEC (IC₅₀=1.8 μM) and A549 cells (IC₅₀=14.8 μM).
Rostafuroxin displaced [³H]Ouabain from the dog kidney Na⁺,K⁺-ATPase receptor (IC50=1.5 nM), is devoid of cardiac inotropic activity in isolated guinea pig atria, and shows no affinity up to 10^-4 M with general (R1, R2, a1, a2, A1, A2, M1, M2, H1, H2, 5-HT1, 5-HT2, Ca2+ channels, TXA2/PGH2, PAF, GABAA, GABAB, DA-NE-5-HT uptake, glutammate,glycine, benzodiazepine) and hormonal (estrogenic, progestinic, androgenic, mineralcorticoid) receptors.

In Vivo: Rostafuroxin (PST 2238; 1 mg/kg/day; gavage; for 3 weeks) decreases SBP and improves acetylcholine-induced relaxation.

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